Drug intelligence / Profile preview

cabozantinib + olaparib

Development stage
Unknown
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

Cabozantinib + olaparib is a combination of two small molecule drugs used in oncology research and clinical trials. Cabozantinib is a multi-targeted tyrosine kinase inhibitor that blocks several receptor tyrosine kinases involved in tumor growth, angiogenesis, and metastatic progression, including MET, VEGFR2, AXL, and RET. Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor that impairs DNA repair by inhibiting PARP enzymes, leading to cell death in cancer cells with deficient homologous recombination repair mechanisms such as those with BRCA mutations. This combination aims to exploit complementary mechanisms—targeting both tumor cell survival pathways and DNA repair—to enhance antitumor efficacy. Both drugs are approved individually for various cancers; their combination is under investigation for synergistic effects in solid tumors.

Other names
XL184 (for cabozantinib)AZD2281 (for olaparib)
02

Targets

AXL (AXL receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)PARP2 (Poly (adp-ribose) polymerase 2)

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